21766-81-4Relevant academic research and scientific papers
Three in one: prototropy-free highly stable AADD-type self-complementary quadruple hydrogen-bonded molecular duplexes with a built-in fluorophore
Kheria, Sanjeev,Rayavarapu, Suresh,Kotmale, Amol S.,Sanjayan, Gangadhar J.
supporting information, p. 2689 - 2692 (2017/03/10)
This communication reports an effective approach for addressing the prototropy-related problems in heterocycle-based AADD-type self-assembling systems by freezing their hydrogen-bonding codes, by utilizing intramolecular bifurcated hydrogen bonding interactions. Using this strategy, we have also developed a hydroquinone-conjugated AADD-type self-assembling system adorned with three valuable features such as prototropy-free dimerization yielding single duplexes, high duplex stability and a built-in fluorophore, which would augment its application potential. The rational approach used herein to arrest prototropic shift may also find application elsewhere, wherein proton shift-mediated structural changes become a detrimental factor.
SAR studies of epoxycurcuphenol derivatives on leukemia CT-CD4 cells
Galindo, José L.G.,Macías, Mariola,Molinillo, José M.G.,Mu?oz-Suano, Alba,Torres, Ascensión,Varela, Rosa M.,García-Cozar, Francisco,Macías, Francisco A.
supporting information, p. 6662 - 6668 (2013/01/15)
Bioactive natural products are a potential source of new pharmaceuticals since they offer new modes of action and more specific activities. The use of derivatization also enables the optimal structure for their biological activity to be determined. In thi
Design, synthesis and SAR study of hydroxychalcone inhibitors of human β-secretase (BACE1)
Ma, Lei,Yang, Zhengyi,Li, Chenjing,Zhu, Zhiyuan,Shen, Xu,Hu, Lihong
experimental part, p. 643 - 648 (2012/04/10)
According to the structural characteristics of isoliquiritigenin from Glycyrrhiza uralensis, a series of hydroxychalcones has been designed, synthesized and evaluated for their in vitro inhibitory activities of β-secretase (BACE1). Structure-activity relationship study suggested that inhibitory activity against BACE1 was governed to a greater extent by the hydroxyl substituent on A-and B-ring of the chalcone, and the most active compound was substituted with four hydroxyl group (17, IC50=0.27 μM).
HYDROQUINONE DERIVATIVES
-
Page/Page column 28, (2010/11/18)
Compounds of general formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8 and R9 have the meanings given in the specification, are useful in the treatment o
NEW COMPOUNDS, WHICH ARE POTENT INHIBITORS OF NA/CA EXCHANGE MECHANISM AND ARE USEFUL IN THE TREATMENT OF ARRHYTHMIAS
-
Page/Page column 36, (2010/02/11)
Therapeutically active compounds of formula (I): wherein X is -O-, -CH2- or -C(O)-; Z is -CHR9- or valence bond; Y is -CH2-, -C(O)-, CH(OR10)-, -CH(NR11R12 )-, -O-, -S-, -S(O)- or -S(O2)-, provided that in case Z is a valence bond, Y is not C(O); the dashed line represents an optional double bond in which case Z is -CR9- and Y is -CH-, C(OR10)- or -C(NR11R12 )-; R1 is -(CH2)nNR4R7 or one of the following groups:n is 1 - 4; R2 and R3 are independently H, lower alkyl, lower alkoxy, -NO2, halogen, -CF3, -OH, -NHR8 or -COOH; R4 and R7 are independently H, lower alkyl or lower hydroxyalkyl; R5 is H, lower alkoxy, -CF3, -NH2 or -CN; R6 is -NO2 , -NR14R19, -CF3 or R8 and R16 are independently H or acyl; R9 is H or lower alkyl; R10 is H, alkylsulfonyl or acyl; R11 and R12 are independently H, lower alkyl or acyl; R13 and R18 are independently H or -OR20; R14 and R19 are independently H, acyl, alkylsulfonyl, C(S)NHR17 or C(O)NHR17; R15 is H or NH2; R17 is H or lower alkyl; R20 is H or acyl; and pharmaceutically acceptable salts and esters thereof are disclosed. The compounds are potent inhibitors of Na/Ca exchange mechanism.
PYRIDINE DERIVATIVES USEFUL FOR INHIBITING SODIUM/CALCIUM EXCHANGE SYSTEM
-
Page 38, (2008/06/13)
Therapeutically active compounds of formula (I) or (II) wherein X is -O-, -CH2- or -C(O)-; Z is -CHR12- or a valence bond; Y is -CH2-, -C(O)-, CH(OR13)-, -O-, -S-; provided that in case Z is a valence bond, Y is not C(O); the dashed line representing an optional double bond in which case Z is -CR12- -and Y is -CH2-, -C(O)- or -CH(OR10)- (in formula II) or -CH- (in formula I); R2 and R3 are independently H, lower alkyl, lower alkoxy, -NO2, halogen, -CF3, -OH, benzyloxy or a group of formula (IIIa). R1 is H, CN, halogen, -CONH2, -COOR15, CH2NR15R18, NHC(O)R5, NHCH2R5, NHR20, NR21R22, NHC(NH)NHCH3 or, in case the compound is of formula (II) wherein the optional double bond exists or in case R2 or R3 is benzyloxy or a group of formula (IIIa) or in case the pyridine ring of formula (I) or (II) is attached to the oxygen atom in 3-, 4- or 5-position, R1 can also be -NO2 or NR16R17; R4 is H, -NO2, CN, halogen, -CONH2, -COOR15, -CH2NR15R18, -NR16R17, NHC(O)R5 or -NHC(NH)NHCH3; R5 is alkyl substituted with 1-3 substituents selected from the group consisting of halogen, amino and hydroxy, or carboxyalkyl, in which the alkyl portion is optionally substituted with 1-3 substituents selected from the group consisting of halogen, amino and hydroxyl, -CHR6NR,R8 or one of the following groups: formula (IVa), (IVb), (IVc), (IVd), (IVe), and pharmaceutically acceptable salts and esters thereof. The compounds are potent inhibitors of Na+/Ca2+ exchange mechanism.
The asymmetric synthesis of 2-benzopyrans and their quinones through intramolecular diastereoselective ring-closure of titanium phenolates of phenolic aldehydes
Giles, Robin G. F.,Joli, Cynthia A.
, p. 3039 - 3048 (2007/10/03)
Treatment of the phenolic aldehyde (a′5,25)-2-(5′-hydroxy-2′-methoxy-a′-methylbenzyloxy) propanal 15 with titanium tetraisopropoxide followed by ultrasonication led to its completely diastereoselective cyclisation in high yield to afford (lS,3S′,4.R)-3,4-
Benzopyran derivatives and an anti-allergic agent possessing the same as the active ingredient
-
, (2008/06/13)
The present invention relates to an extremely effective anti-allergic agent with a low toxicity, which possesses as its active ingredient a benzopyran derivative described by the general formula below (in the formula, R1 and R2 are each respectively a hydrogen atom, an acyl group, an alkyl group having 1?12 carbon atoms, or an alkenyl group having 2?10 carbon atoms; and R3 is a hydroxyl group, an acyloxy group, an alkoxy group having 1?10 carbon atoms, or an alkenyloxy group having 2?10 carbon atoms). General Formula STR1
Synthetic aci-Reductones: 3,4-Dihydroxy-2H-1-benzopyran-2-ones and Their cis- and trans-4a,5,6,7,8,8a-Hexahydro Diastereomers. Antiaggregatory, Antilipidemic, and Redox Properties Compared to Those of the 4-Substituted 2-Hydroxytetronic Acids
Witiak, Donald T.,Kim, Sung K.,Tehim, Ashok K.,Sternitzke, Kent D.,McCreery, Richard L.,et al.
, p. 1437 - 1445 (2007/10/02)
Synthetic procedures for the elaboration of aci-reductones belonging to the 6- or 7-mono- or bis-substituted-3,4-dihydroxy-2H-1-benzopyran-2-ones (6 - 10) and their cis- and trans-4a,5,6,7,8,8a-hexahydro diastereomers (11, 12) are described.Hexahydrobenzo
